Description:
Given the proposed involvement of VLA-4 in inflammatory processes, a program to identify orally active VLA-4 antagonists was initiated. Herein, we report the discovery of a N -tetrahydrofuroyl-( l )-phenylalanine derivative ( 17 ) and related analogues as potent VLA-4 antagonists with good oral bioavailability. The synthesis, biological properties, and pharmacokinetic profile of tetrahydrofuranoyl such as 17 are reported.